METHOD FOR MANUFACTURING OF SUBSTANCES WITH -NH2 P WHICH ARE RELEASED FROM POLYMERS BY ENZYMES

摘要

The present invention relates to a method of manufacturing a macromolecular form of active substances with -NH2 groups which is useful for protracted release of the active component by an enzymatic cleavage, wherein an N-substituted amide or ester of acrylic or methacrylic acid, which contains at least three chained atoms in its side chain terminated by the carboxylic carbon atom, is condensed with the.alpha.-amine group of an aminoacid of L-configuration, as .beta.-phenylalanine, tyrosine, tryptophan, lysine, arginine, glycine, alanine, leucine, citrulline or ornithine, and then an active component is bonded by its -NH2 groups to the carboxylic group of this amino acid and the resulting monomer is copolymerised with a hydrophilic monomeric component based on N-alkymethyacrylamide, N-alkyacrylamide, N,N-dialkylacrylamide where alkyl has 1 to 6 carbon atoms and may contain 1 to 3 -OH groups, or glycol methacrylate or glycol acrylate, where glycol is ethylene glycol, propylene glycol, butylene glycol, diethylene glycol, triethylene glycol and tetraethylene glycol, alone or in a mixture, and if desired with further monomeric components which may act as crosslinking agent. The polymeric form prepared by the method according to the present invention enables to control the physical and biological fate of the active substance by the nature and molecular weight of the carrier-polymer.